86580-67-8Relevant academic research and scientific papers
PYRIMIDINE JAK INHIBITORS FOR THE TREATMENT OF SKIN DISEASES
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Page/Page column 39-40, (2020/11/04)
The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory and autoimmune skin diseases.
ESTER AND CARBONATE PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS
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Page/Page column 36-38, (2020/11/03)
The invention provides compounds of formula (I): (I) or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases and release an active metabolite in vivo. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory skin diseases and other diseases.
PYRIMIDINE COMPOUND AS JAK KINASE INHIBITOR
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Paragraph 0231; 0236-0237, (2019/05/15)
The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography
Mach,Leudtke,Unsworth,Boundy,Nowak,Scripko,Elder,Jackson,Hoffman,Evora,Rao,Molinoff,Childers,Ehrenkaufer
, p. 3707 - 3720 (2007/10/02)
Two series of (N-benzylpiperidin-4-yl)- and (9-azabicyclo[3.3.1]nonan- 3β-yl)benzamides were prepared, and in vitro binding assays were used to measure the affinity of these compounds for dopamine D2, dopamine D3, serotonin 5-HT2, and α2-adrenergic receptors. The results of these studies indicated compounds 23, 26b, and 34 have the selectivity needed for in vivo studies of the D2 (and possibly D3) receptors. 18F-Labeled analogues of 23, 26b and 34 were prepared by N-alkylation of the corresponding desbenzyl precursors with [18F]-4-fluorobenzyl iodide. Preliminary in vivo studies demonstrated that [18F]-23 and [18F]-26b are suitable candidates for further evaluation in positron emission tomography imaging studies. The slow rate of washout of [18F]-34 from nondopaminergic regions and its comparatively high lipophilicity indicates that this compound may not be suitable for imaging studies because of a high level of nonspecific binding.
